Recent HOT MedChemComm articles

The following MedChemComm articles have all been recommened by the reviewers of the articles as being particularly interesting or particularly significant research. These have all been made free to access until 12th December 2014. The order they appear in the list holds no special meaning or ranking.

Imidazole derivatives show anticancer potential by inducing apoptosis and cellular senescence
Gangavaram V. M. Sharma, Adepu Ramesh, Ashita Singh, Gourishetty Srikanth, Vankudoth Jayaram, Divya Duscharla, Jung Ho Jun, Ramesh Ummanni and Sanjay V. Malhotra  
DOI: 10.1039/C4MD00277F, Concise Article

C4MD00277F


Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor
Katherine S. England, Anthony Tumber, Tobias Krojer, Giuseppe Scozzafava, Stanley S. Ng, Michelle Daniel, Aleksandra Szykowska, KaHing Che, Frank von Delft, Nicola A. Burgess-Brown, Akane Kawamura, Christopher J. Schofield and Paul E. Brennan  
DOI: 10.1039/C4MD00291A, Concise Article
From themed collection Epigenetics

C4MD00291A GA


Computationally motivated synthesis and enzyme kinetic evaluation of N-(β-D-glucopyranosyl)-1,2,4-triazolecarboxamides as glycogen phosphorylase inhibitors
Jaida Begum, Gergely Varga, Tibor Docsa, Pál Gergely, Joseph M. Hayes, László Juhász and László Somsák  
DOI: 10.1039/C4MD00335G, Concise Article

C4MD00335G GA


Synthesis and biological evaluation of a series of aryl triazoles as firefly luciferase inhibitors
Haixiu Bai, Peng Zhu, Wenxiao Wu, Jing Li, Zhao Ma, Wei Zhang, Yanna Cheng, Lupei Du and Minyong Li  
DOI: 10.1039/C4MD00368C, Concise Article

C4MD00368C GA


Rational design of protein–protein interaction inhibitors
Didier Rognan  
DOI: 10.1039/C4MD00328D, Review Article

C4MD00328D GA

 

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

Q2 Top Ten most accessed articles

The 10 most accessed MedChemComm articles between April and June 2014

During the months April – June 2014, the most downloaded MedChemComm articles were:

The synthesis and functional evaluation of a mitochondria-targeted hydrogen sulfide donor, (10-oxo-10-(4-(3-thioxo-3H-1,2-dithiol-5- yl)phenoxy)decyl) triphenyl phosphonium bromide (AP39)
Sophie Le Trionnaire, Alexis Perry, Bartosz Szczesny, Csaba Szabo, Paul G. Winyard, Jacqueline L. Whatmore, Mark E. Wood and Matthew Whiteman
DOI: 10.1039/C3MD00323J

Emerging classes of armed antibody therapeutics against cancer
Christian Hess, Dario Venetz and Dario Neri
DOI: 10.1039/C3MD00360D

The role of modern drug discovery in the fight against neglected and tropical diseases
Jeremy N. Burrows, Richard L. Elliott, Takushi Kaneko, Charles E. Mowbray and David Waterson
DOI: 10.1039/C4MD00011K

Discovery of BET bromodomain inhibitors and their role in target validation
S. Müller and S. Knapp
DOI: 10.1039/C3MD00291H

Identification of an inhibitor of the ubiquitin–proteasome system that induces accumulation of polyubiquitinated proteins in the absence of blocking of proteasome function
Caroline Haglund, Chitralekha Mohanty, Mårten Fryknäs, Padraig D’Arcy, Rolf Larsson, Stig Linder and Linda Rickardson
DOI: 10.1039/C3MD00386H

Ambient mass spectrometry technologies for the detection of falsified drugs
María J. Culzoni, Prabha Dwivedi, Michael D. Green, Paul N. Newton and Facundo M. Fernández
DOI: 10.1039/C3MD00235G

Affinity-based target identification for bioactive small molecules
Makoto Kawatani and Hiroyuki Osada
DOI: 10.1039/C3MD00276D

Fragment growing to retain or alter the selectivity of anchored kinase hinge-binding fragments
Charlotte E. Allen, Amanda J. Welford, Thomas P. Matthews, John J. Caldwell and Ian Collins
DOI: 10.1039/C3MD00308F

Two diseases, one approach: multitarget drug discovery in Alzheimer’s and neglected tropical diseases
F. Prati, E. Uliassi and M. L. Bolognesi
DOI: 10.1039/C4MD00069B

FP tethering: a screening technique to rapidly identify compounds that disrupt protein–protein interactions
Jean M. Lodge, T. Justin Rettenmaier, James A. Wells, William C. Pomerantz and Anna K. Mapp
DOI: 10.1039/C3MD00356F

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

Recent HOT MedChemComm articles

The following are HOT articles, as recommened by the reviewers of the articles. These have all been made free to access until 24th October:

Structure-based approaches towards identification of fragments for the low-druggability ATAD2 bromodomain
Apirat Chaikuad, Andrew M. Petros, Oleg Fedorov, Jing Xu and Stefan Knapp
Med. Chem. Commun., DOI: 10.1039/C4MD00237G, Concise Article
From themed collection Epigenetics


Gold compounds as aquaporin inhibitors: new opportunities for therapy and imaging
Andreia de Almeida, Graça Soveral and Angela Casini
Med. Chem. Commun., DOI: 10.1039/C4MD00265B, Review Article


A novel surface-coated nanocarrier for efficient encapsulation and delivery of camptothecin to cells
Rie Wakabayashi, Ryutaro Ishiyama, Noriho Kamiya and Masahiro Goto
Med. Chem. Commun., DOI: 10.1039/C4MD00179F, Concise Article
From themed collection In celebration of Seiji Shinkai’s 70th Birthday


Peptide HIV fusion inhibitors: modifications and conjugations
Wei Liu, Jianjun Tan, Mohammadreza Mohammadzad Mehryar, Zhiping Teng and Yi Zeng
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00214H, Review Article


3,5-Diamino-1,2,4-triazoles as a novel scaffold for potent, reversible LSD1 (KDM1A) inhibitors
Craig J. Kutz, Steven L. Holshouser, Ethan A. Marrow and Patrick M. Woster
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00283K, Concise Article
From themed collection Epigenetics

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

Christian Heinis receives MedChemComm Lectureship at EFMC-ISMC

Christian Heinis with MedChemComm Managing Editor Richard Kelly. Photograph: Fabien Venturi

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

Medicinal Chemistry Residential School comes to Asia

Registration now open for Medicinal Chemistry Residential School 2014

With a 40 year history in the UK, the Royal Society of Chemistry Medicinal Chemistry Residential School has trained some of the world’s leading medicinal chemists working in the pharmaceutical industry. Now, for the first time, this highly successful course will be coming to Asia – from 20-23 November, Shangai, China.

Do you want to develop your medicinal chemistry skills?

This 3-day course strengthens excellence in medicinal chemistry by highlighting best practice and facilitating understanding of the factors governing modern drug discovery.

What you will learn

The course covers all aspects of drug discovery. A full list of themes is on our website. These topics will be explored through a varied programme of lectures, case histories, and hands-on tutorial sessions.

Who you will learn from

This is a truly unique opportunity for discussions and networking with peers and internationally recognised leaders in the field. See our list of prestigious speakers.

Registration is now open. There are limited spaces available on the course so make sure you register as soon as possible.

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

Recent HOT MedChemComm articles

Check out the following HOT articles, these have been made free to access for a limited time:

Recognition of diazirine-modified O-GlcNAc by human O-GlcNAcase
Andrea C. Rodriguez and Jennifer J. Kohler
Med. Chem. Commun., 2014,5, 1227-1234
DOI: 10.1039/C4MD00164H

Recognition of diazirine-modified O-GlcNAc by human O-GlcNAcase

Free to access until 21st August 2014


Evaluation of functional groups as acetyl-lysine mimetics for BET bromodomain inhibition
Phillip P. Sharp, Jean-Marc Garnier, David C. S. Huang and Christopher J. Burns
Med. Chem. Commun., 2014, Advance Article
DOI: 10.1039/C4MD00182F

Evaluation of functional groups as acetyl-lysine mimetics for BET bromodomain inhibition

Free to access until 21st August 2014


Beyond substrate analogues: new inhibitor chemotypes for glycosyltransferases
Lauren Tedaldi and Gerd K. Wagner
Med. Chem. Commun., 2014,5, 1106-1125
DOI: 10.1039/C4MD00086B

Beyond substrate analogues: new inhibitor chemotypes for glycosyltransferases

Free to access until 21st August 2014

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

RSC Organic Division Poster Symposium 2014

RSC Organic Division Poster Symposium 2014, headline sponsored by F. Hoffmann-La Roche, Ltd.

The poster symposium, for final year organic chemistry PhD students, will take place at The Royal Society of Chemistry, Burlington House, London on Monday 01 December 2014.

The symposium offers final year PhD students a chance to showcase their research to their peers, leading academics and industrial chemists, and is open to all branches of organic chemistry. The symposium has a tradition of being the most competitive and highly regarded organic chemistry symposium for PhD students in the UK and ROI and we would like to thank F. Hoffmann-La Roche, Ltd. for their generous support of the event.

There will be a first prize of £500, two runner-up prizes of £250, and a “selected by Industry Prize”. Industrial delegates will make this selection by considering the research’s potential for application in an industrial context; the winner will also receive a prize of £500.

Closing date for submissions is Wednesday 01 October 2014.
For more information and to submit your abstract go to http://rsc.li/organic-poster

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

European Federation for Medicinal Chemistry (EFMC) Awards

Every two years the European Federation for Medicinal Chemistry (EFMC), a partner society of MedChemComm, honour three awards at the International Symposium on Medicinal Chemistry (EFMC-ISMC).  Congratulations to the following winners of the EFMCEFMC Awards 2014!

Nauta Award for Pharmacochemistry
Professor Paul Leeson
GlaxoSmithKline, UK

UCB-Ehrlich Award for Excellence in Medicinal Chemistry
Professor Craig Crews
Yale University, Department of Chemistry, New Haven, USA

Prous Institute-Overton and Meyer Award for New Technologies in Drug Discovery
Professor György Ferenczy and Professor György Keseru
Research Centre for Natural Sciences, Hungarian Academy of Sciences, Budapest, Hungary

These awards acknowledge outstanding achievements in the field of Medicinal Chemistry.

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

Make your journal work for you

Find out how to get the most from MedChemComm

Want to know about the latest research we publish in MedChemComm? Want to be told about upcoming themed issues, or the most read articles, or other journal news?

Here are a few ways you can stay in touch with us and all that is happening:

RSS Feed for MedChemCommMost recent articles

Be informed about the latest articles published on our website by adding us to your RSS Feed.


Issue alerts

Sign-up to MedChemComm issue alertsGet the table of contents of the latest issue of MedChemComm sent direct to you when we publish the issue.


News alerts

Register for MedChemComm news alertsBy joining our news alerts we can let you know about:

  • Up-coming themed collections (print & electronic)
  • Top Ten most accessed articles
  • Changes to our Editorial Board
  • Important news for the journal


Twitter

We can also be found on Twitter @MedChemComm, add us and say hello. MedChemComm twitter


And of course you can always come back to this blog to find out about our journal news.

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)

Kinase 2014

A very successful Kinase 2014 was held on 19-20 May 2014 with some great talks and interesting perspectives being presented on the future of kinase inhibitor research.

Kinase 2014 Chinese Pharmaceutical Association delegation

Kinase 2014 CPA delegation

Eight VIP Chinese Pharmaceutical Association (CPA) delegates attended the Kinase 2014 held at the Babraham Research Institute in Cambridge. Three of the CPA delegates presented their research at the meeting which also included a lecture from Nathanael S Gray (Harvard), recent guest editor for Med Chem Comm themed issue “Chemical Biology for Target Identification and Validation”.

Along with the talks a series of posters were also presented. Two of these recieved Poster Prizes sponsored by the Chemistry Biology Interface Division (CBID) and MedChemComm.

Jeff Kropf (Gilead Sciences) won the MedChemComm prize for his research on the discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase (Syk).

Charlotte Griffiths-Jones (Astex Pharmaceuticals) won the CBID prize for her poster on fragment based drug discovery of selective inhibitors of fibroblast growth facter receptor (FGFR).

MedChemComm poster prize at Kinase 2014

Jeff Kropf being presented with his poster prize

Charlotte Griffiths-Jones being presented with her CBID prize at Kinase 2014

Charlotte Griffiths-Jones being presented with her CBID prize

Digg This
Reddit This
Stumble Now!
Share on Facebook
Bookmark this on Delicious
Share on LinkedIn
Bookmark this on Technorati
Post on Twitter
Google Buzz (aka. Google Reader)